GDC0276 manufacturers
- GDC-0276
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- $0.00 / 1removed
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2026-04-16
- CAS:1494581-70-2
- Min. Order:
- Purity: 99.77%
- Supply Ability: 10g
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| | GDC0276 Basic information |
| Product Name: | GDC0276 | | Synonyms: | GDC0276;GDC0276,GDC 0276;Benzamide, N-(1-azetidinylsulfonyl)-5-cyclopropyl-2-fluoro-4-(tricyclo[3.3.1.13,7]dec-1-ylmethoxy)-;4-(Adamantan-1-ylmethoxy)-N-(azetidin-1-ylsulfonyl)-5-cyclopropyl-2-fluorobenzamide;4-(1-Adamantylmethoxy)-N-(azetidin-1-ylsulfonyl)-5-cyclopropyl-2-fluorobenzamide | | CAS: | 1494581-70-2 | | MF: | C24H31FN2O4S | | MW: | 462.58 | | EINECS: | | | Product Categories: | | | Mol File: | 1494581-70-2.mol |  |
| | GDC0276 Chemical Properties |
| density | 1.39±0.1 g/cm3(Predicted) | | form | Solid | | pka | 4.17±0.20(Predicted) | | color | White to off-white |
| | GDC0276 Usage And Synthesis |
| Description | GDC0276, also known as RG7893, is a selective, reversible, orally bioavailable small-molecule sodium channel blocker that is selective for Nav1.7, which is expressed primarily on peripheral nociceptor C-fiber neurons and is required for pain sensing in humans. | | Uses | GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects[1]. | | in vivo | GDC-0276 (oral adminstration; 0.5-5 mg/kg) shows enrichment of 14C with observed specific activities of 22.6 μCi/mg. GDC-0276 is not detected in urine; however, metabolites in urine were enriched in 14C with observed specific activities of 19.6 μCi/mg[3]. | Animal Model: | Six drug-nave beagle dogs Group 1 four dogs (n=2 per sex) and Group 2 2 BDC dogs (n=2 male)[3] | | Dosage: | 0.5, 1, 2, 3, 4, 5 mg/kg | | Administration: | Oral adminstration | | Result: | Showed mean specific activities of 12.2 μCi/mg (a 24% enrichment) (n=4 animals) and 23.5 μCi/mg (a 139% enrichment) (n=2 animals) for Groups 1 and 2, respectively. |
| | IC 50 | Nav1.7 | | References | [1] Rothenberg ME, et al. Safety, Tolerability, and Pharmacokinetics of GDC-0276, a Novel NaV1.7 Inhibitor, in a First-in-Human, Single- and Multiple-Dose Study i DOI:10.1007/s40261-019-00807-3
[2] Steven J. McKerrall, et al. Nav1.7 inhibitors for the treatment of chronic pain. Bioorganic & Medicinal Chemistry Letters (2018)
[3] Takahashi RH,et al.Unequal Absorption of Radiolabeled and Nonradiolabeled Drug from the Oral Dose Leads to Incorrect Estimates of Drug Absorption and Circulating Metabolites in a Mass Balance Study.Drug Metab Lett. 2019;13(1):37-44. DOI:10.2174/1872312813666181129162237 |
| | GDC0276 Preparation Products And Raw materials |
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